LY341495

Names

[ CAS No. ]:
201943-63-7

[ Name ]:
LY341495

[Synonym ]:
(1S,2S)-2-[(1S)-1-Amino-1-carboxy-2-(9H-xanthen-9-yl)ethyl]cyclopropanecarboxylic acid
9H-Xanthene-9-propanoic acid, α-amino-α-[(1S,2S)-2-carboxycyclopropyl]-, (αS)-
cc-481
HMS3267B15
LY-341,495
Z99
LY341495

Biological Activity

[Description]:

LY341495 is a metabotropic glutamate receptor (mGluR) antagonist with IC50s of 2.9 nM, 10 nM, 170 nM for mGluR-2, mGluR-3, mGluR-8, respectively.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> mGluR

Research Areas >> Neurological Disease

[Target]

IC50: 2.9 nM (mGluR-2, human), 10 nM (mGluR-3, human), 170 nM (mGluR-8, human)

[In Vivo]

LY341495 (0.3, 1, and 3 mg/kg, i.p.) displays a lower level of discrimination in rats[1]. LY341495 (3.0 mg/kg) decreases Dvl-2, pGSK-3α/β and β-catenin protein levels but Dvl-1, Dvl-3 and GSK-3α/β are unaffected in both the PFC and STR. LY341495 has the generally the opposite effect following acute and chronic administration compared to mGlu2/3 agonist, LY379268[2]. LY341495 (3 mg/kg, i.p., 2.5 h) -induced c-Fos expression is not altered in either KO brain. LY341495 is almost inactive in the central extended amygdala [central nucleus of the amygdala, lateral (CeL) and bed nucleus of the stria terminalis, laterodorsal (BSTLD)] in mGluR3-KO mice[3].

[Animal admin]

The rats are randomLy divided into six experimental groups (10 rats per group): vehicle and 0.05, 0.1, 0.3, 1, and 3 mg/kg LY341495. The LY341495 doses are selected on the basis of results from previous Published studies that evaluated the effects of this compound on cognition. The rats are subjected to a training session that consisted of two 2-min trials. The animals receive either vehicle or LY341495 immediately after T1. Using the 2-min trial duration, an ITI of 1 h is used because recognition memory is still intact in untreated control rats under these experimental conditions

[References]

[1]. Pitsikas N, et al. The metabotropic glutamate 2/3 receptor antagonist LY341495 differentially affects recognition memory in rats. Behav Brain Res. 2012 May 1;230(2):374-9.

[2]. Sutton LP, et al. Regulation of Akt and Wnt signaling by the group II metabotropic glutamate receptor antagonist LY341495 and agonist LY379268.J Neurochem. 2011 Jun;117(6):973-83.

[3]. Linden AM, et al. Use of MGLUR2 and MGLUR3 knockout mice to explore in vivo receptor specificity of the MGLUR2/3 selective antagonist LY341495. Neuropharmacology. 2009 Aug;57(2):172-82. Epub 2009 May 27.

[4]. Li J, et al. N-acetyl-cysteine attenuates neuropathic pain by suppressing matrix metalloproteinases. Pain. 2016 Aug;157(8):1711-23.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
580.8±40.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₀H₁₉NO₅

[ Molecular Weight ]:
353.369

[ Flash Point ]:
305.1±27.3 °C

[ Exact Mass ]:
353.126312

[ PSA ]:
109.85000

[ LogP ]:
2.53

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.669

[ Storage condition ]:
2-8℃